Braga P C, Dal Sasso M, Maci S, Piatti G, Dannhorn D R, Bohn M
Department of Pharmacology, School of Medicine, University of Milan, Italy.
Arzneimittelforschung. 1995 Jan;45(1):84-7.
Candida albicans is an opportunistic dimorphic pathogenic yeast which is present on the human mucosal epithelial cell surface. Its adhesion is considered to be an important first step in colonization and in the subsequent symptomatic or asymptomatic infection of buccal or vaginal mucosa. Because the ability to adhere is an important element of the pathogenicity of Candida we investigated in this study the compared effects of sub-inhibitory concentrations (sub-MICs) of rilopirox (CAS 104153-37-9) with those of ciclopirox olamine (CAS 41621-49-2) in inhibiting Candida adhesion to human buccal (BEC) and vaginal cells (VEC). Rilopirox is a new hydroxypyridone antimycotic agent with strong activity, especially against Candida albicans. There was a significant reduction in the mean number of Candida adhering to both buccal and vaginal cells with up to 1/8 MIC rilopirox for buccal and 1/16 MIC for vaginal cells, while for ciclopirox olamine reduction was significant up to 1/16 MIC for buccal and 1/8 MIC for vaginal cells. There were no significant differences in the dose-effect curves for BEC and VEC with either rilopirox and ciclopirox olamine, but on a molar basis, rilopirox was more active than ciclopirox olamine. The present in-vitro results support the developmental concept of an oropharyngeal and vaginal preparation of rilopirox. It can be expected that even sub-inhibitory concentrations of rilopirox exert an important additional effect in the treatment of oral and vaginal candidosis by impairing the pathogenic adhesion process of the fungus.
白色念珠菌是一种机会性双态致病酵母,存在于人类黏膜上皮细胞表面。其黏附被认为是在颊黏膜或阴道黏膜定植以及随后发生有症状或无症状感染的重要第一步。由于黏附能力是念珠菌致病性的一个重要因素,我们在本研究中调查了利洛吡罗(CAS 104153-37-9)和环吡酮胺(CAS 41621-49-2)的亚抑制浓度(亚 MIC)对抑制念珠菌黏附人颊细胞(BEC)和阴道细胞(VEC)的比较效果。利洛吡罗是一种新型羟基吡啶酮抗真菌剂,具有较强活性,尤其对白色念珠菌。对于颊细胞,使用高达 1/8 MIC 的利洛吡罗,对于阴道细胞,使用高达 1/16 MIC 的利洛吡罗,黏附到颊细胞和阴道细胞上的念珠菌平均数量均显著减少;而对于环吡酮胺,对于颊细胞,高达 1/16 MIC 时减少显著,对于阴道细胞,高达 1/8 MIC 时减少显著。利洛吡罗和环吡酮胺对 BEC 和 VEC 的剂量效应曲线没有显著差异,但以摩尔计,利洛吡罗比环吡酮胺更具活性。目前的体外研究结果支持开发利洛吡罗的口咽和阴道制剂的理念。可以预期,即使是利洛吡罗的亚抑制浓度,也能通过损害真菌的致病性黏附过程,在治疗口腔和阴道念珠菌病方面发挥重要的额外作用。